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Target intelligence / Profile preview
Euchromatic histone lysine methyltransferase 2 (G9A)
- Target
- G9A
- Molecular classification
- Protein, Enzyme, Histone lysine methyltransferase, Transcription factor, Histone modification
01
Overview
Euchromatic histone lysine methyltransferase 2 (G9A), also known as EHMT2 or KMT1C, is a nuclear enzyme that plays a central role in epigenetic regulation through the methylation of histone and non-histone proteins. G9A primarily catalyzes mono-, di-, and to a lesser extent tri-methylation of lysine 9 on histone H3 (H3K9me1/2/3), which is generally associated with transcriptional repression. Elevated levels or dysregulation of G9A are implicated in various cancers. Selective inhibition of G9A has been shown experimentally to reduce cancer cell proliferation, making it an attractive target for anticancer drug development.
- Other names
- EHMT2KMT1C
02
Mechanism of action
Inhibition of H3K9 methylation
03
Biological functions
Histone methylationGene regulationTranscriptional repressionTranscriptional coactivationRegulation of T-cell differentiationRegulation of immune responsesRegulation of neural plasticityRegulation of DNA repairProviral silencing
04
Disease associations
CancerInflammatory diseasesIBD
05
Interacting drugs
BIX-01294
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